兰索拉唑肠溶微丸的制备及质量研究

Preparation and Quality Research of Lansoprazole Enteric-coated Pellets

目的制备兰索拉唑肠溶微丸,以提高难溶性药物兰索拉唑的耐酸力、释放度及稳定性。方法采用粉末层积微丸制备方法,结合离心造粒及流化床包衣技术制备兰索拉唑肠溶微丸。以兰索拉唑肠溶胶囊TAKEPRON为参比制剂,考察自制制剂和参比制剂的微丸性能、释放度及影响因素稳定性,并采用相似因子比较法,评价自制制剂与参比制剂的体外释放一致性。结果制备的兰索拉唑肠溶微丸呈白色球形且粒径分布均匀,圆整度好,耐磨损能力强,与参比制剂在不同pH介质中的释放度相似因子均>50。在影响因素条件下,自制制剂与参比制剂的含量变化趋势相同,但自制制剂的有关物质变化程度低于参比制剂。结论本研究制备的兰索拉唑肠溶微丸可以有效提高兰索拉唑的耐酸力,改善兰索拉唑在不同pH介质中的释放度,达到与参比制剂在模拟肠液中的释放一致性。相较于参比制剂,自制兰索拉唑肠溶微丸的稳定性相较于参比制剂有所提高。

OBJECTIVE To prepare lansoprazole enteric-coated pellets,so as to improve the acid resistance,release and stability of lansoprazole.METHODS The lansoprazole enteric-coated pellets were prepared by powder laminar deposition technique combing the centrifugal granulator and the fluidized bed coating technology.The commercial lansoprazole enteric-coated capsules(TAKEPRON)were selected as reference formulation.The performance,release,stability and influencing factors of self-made formulation and reference formulation were investigated.The release consistency of the lansoprazole enteric-coated pellets with the reference formulation was evaluated by the similar factor comparison.RESULTS The prepared lansoprazole enteric-coated pellets were white and sphere with uniform particle size distribution,which had good roundness and strong abrasion resistance.The similarity factors with the reference formulation in the different pH media were all above 50.Under the conditions of influencing factors,the content change trend of self-made formulation was as same as reference formulation,but the change degree of related substances of self-made formulation was lower than reference formulation.CONCLUSION The prepared lansoprazole enteric-coated pellets can effectively improve the acid resistance and release rate of lansoprazole in different pH phosphate buffer solution,and achieve a release consistency with reference formulation in simulated intestinal fluid.Compared with the reference formulation,the stability of lansoprazole enteric coated pellets prepared are improved.